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22 Cards in this Set
- Front
- Back
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A 1% reduction in total cholesterol would equal to how many PERCENT rduction in CHD event?
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2%
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A 10% reduction in population-wide total cholesterol is equal to how many percent reduction in coronary heart disease?
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30%
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What is the primary goal for drug therapy of dyslipidemia?
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reduction of low-density lipoprotein cholesterol (LDL-C) levels
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What are 2 comparably important goal for drug therapy of dyslipidemia?
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elevation of high-density lipoprotein cholesterol (HDL-C) levels and reduction of triglyceride levels
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A 1% reduction in total LDL-C would equal to how man PERCENT reduction in CHD events?
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1%
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A 1% increase in HDL-C would equal to how man PERCENT reduction in CHD events?
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3%
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What is the mechanism of statin?
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It is a competitive inhibitors of HMG-CoA (3 hydroxy-3-methylglutaryl coenzyme A) reductase. Block synthesis of cholesterol in the LIVER.
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How many gram(s) of cholesterol does the human body make a day?
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About 1 gram (1000mg)
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What are the three statins metabolized by CYP3A4?
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atorvastatin, lovastatin, and simvastatin
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What is fluvastatin metabolized by?
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CYP2C9
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Which cytochrome P450 does grapefruit juice inhibit?
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CYP3A4
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Can you use a bile-acid sequestrants as the primary agent for treating dyslipidemia?
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No, they are usually used as second agents if statin monotherapy is not sufficient
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True/False. Bile-acid sequestrants dugs are absorbed from the intestine?
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False, they are not absorbed from the intestine
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What is the mechanism of action for bile-acid sequestrants?
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resins are highly “+” charged & bind “–” charged bile acids; being large macromolecules → are not absorbed in intestines & are eliminated
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Which class of drug is the best agent for increasing HDL-C?
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Niacin
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What is omega-3-acid ethyl esters (Omacor, Lovaza)mainly used for?
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Treatment of hypertriglyceride (>500mg/dl)
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What are the four pleiotropic effects of statin?
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improvement of endothelial function, enhanced production of Nitric Oxide, down regulation of AT1 receptor expression, and inncreased plaque stability
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Which two statins are pro-drugs (need to be metabolized)?
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lovastatin and simvastatin
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Which fibrate drug inhibit CYP2C9-main enzyme metabolizing fluvastatin (crestor)?
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Gemfibrozil
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What class of drug is the best agent for increasing HDL-C level?
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Niacin
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How will Niacin be metabolized and excreted at low dose?
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At low doses metabolized into nicotinuric acid & excreted in urine
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How will Niacin be excreted at high doses?
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At high doses grater proportion is excreted in urine unchanged
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